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    Dolastatin 15 derivatives
    72.
    发明专利
    Dolastatin 15 derivatives 未知

    公开(公告)号：NZ502296A

    公开(公告)日：2002-02-01

    申请号：NZ50229698

    申请日：1998-07-07

    Applicant: BASF AG

    Inventor： JANSSEN BERND ,  BARLOZZARI TERESA ,  HAUPT ANDREAS ,  ZIERKE THOMAS ,  KLING ANDREAS

    IPC: A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  C07K7/06 ,  C12P19/34

    Abstract: Compound of formula: A-B-D-E-F-(G)r-(K)s-L wherein: A is a proline derivative of formula IIa, wherein na is O to 3; Ra I hydrogen, or unsubstituted or fluorine-substituted normal, branched or cyclic C1-3-alkyl; R1a is hydrogen, C1-3 -alkyl, phenyl, or substituted phenyl; or Ra and R1a together form a propylene bridge; and R2a, R3a, R4a and R5a are each, independently, hydrogen or alkyl; or an alpha-amino acid derivative of Formula IIIa, Formula IVa, Formula Va, Formula VIa, Formula VIIa, Formula VIIIa, a 2-azabicyclo heptane-3-carboxylic acid derivative of Formula IXa, an amino acid derivative of Formula Xa; B is a valyl, isoleucyl, allo-isoleucyl, norvalyl, 2-tert-butylglycyl or 2-ethylglycyl residue; or an alpha-amino acid residue of Formula IIb; D is an N-alkylvalyl, N-alkyl-2-ethylglycyl, N-alkyl-2-tert-butylglycyl, N-alkylnorleucyl, N-alkylisoleucyl, N-alkyl-allo-isoleucyl or N-alkylnorvalyl residue; or an alpha-amino acid residue of Formula IId, Formula IIId; E is a prolyl, thiazolidinyl-4-carbonyl, homoprolyl, or hydroxyprolyl residue; or an alpha-amino acid residue of Formula IIe; or an aminocyclopentanecarboxylic acid residue of Formula IIIe, wherein Re is alkyl and R1e is hydrogen, or unsubstituted or fluorine-substituted alkyl; F is a prolyl, thiazolidinyl-4-carbonyl, homoprolyl or hydroxyprolyl residue; or an alpha-amino acid residue of Formula IIf; or a 2- or 3-aminocyclopentanecarboxylic acid residue of Formula IIIf; G is an alpha-amino acid residue of Formula IIg; K is an alpha-amino acid of Formula IIk; and L is a substituted or unsubstituted amino, hydrazido, aminoxy or oximato group; and r and s are independently, 0 or 1; provided that when s and r are 0 and A is of formula IIa where na is 0 or 1 and R1a, R2a, R3a, R4a and R5a are each hydrogen, L is a substituted or unsubstituted amino or hydrazido group .

    Dolastatin 15 derivatives.
    73.
    发明专利
    Dolastatin 15 derivatives. 未知

    公开(公告)号：ZA200100169B

    公开(公告)日：2002-01-08

    申请号：ZA200100169

    申请日：2001-01-08

    Applicant: BASF AG

    Inventor： RITTER KURT ,  JANSSEN BERND ,  HAUPT ANDREAS ,  KLING ANDREAS ,  TERESA BARLOZ-ZARI ,  AMBERG WILHELM

    IPC: A61K38/00 ,  A61K35/56 ,  A61P35/00 ,  C07K5/103 ,  C07K5/117 ,  C07K7/02 ,  C07K ,  A61K

    Abstract: Compounds of the present invention include cell growth inhibitors which are peptides of Formula IA-B-D-E-F-G(I)and acid salts thereof, wherein A, D, and E are alpha -amino acid residues, B is an alpha -amino acid residue or an alpha -hydroxy acid residue, F is an aminobenzoic acid residue or an aminocycloalkanecarboxylic acid residue, and G is a monovalent radical, such as, for example, a hydrogen atom, an amino group, an alkyl group, an alkylene alkyl ether, an alkylene alkyl thioether, an alkylene aldehyde, an alkylene amide, a beta -hydroxylamino group, a hydrazido group, an alkoxy group, a thioalkoxy group, an aminoxy group, an oximato group, an alkylene aryl group, an alkylene ester, an alkylene sulfoxide or an alkylene sulfone. Another aspect of the present invention includes pharmaceutical compositions comprising a compound of Formula I and a pharmaceutically acceptable carrier. An additional embodiment of the present invention is a method for treating cancer in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound of Formula I in a pharmaceutically acceptable composition.

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